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A kind of regorafenib tablet and preparation method thereof

A regorafenib tablet and a technology for regorafenib are applied in the field of preparation of regorafenib tablets and regorafenib tablets, and can solve difficulties in preparation of dosage forms, low bioavailability, and dissolution of active ingredients. problems such as low degree of dissolution, to achieve the effect of good reproducibility, low production cost and high dissolution rate

Active Publication Date: 2019-01-04
HENAN RUNHONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the limited solubility of regorafenib monohydrate (almost insoluble in common solvents), the existing dosage forms have low dissolution rate of active ingredients, low bioavailability, and difficult preparation of dosage forms

Method used

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  • A kind of regorafenib tablet and preparation method thereof
  • A kind of regorafenib tablet and preparation method thereof
  • A kind of regorafenib tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] The regorafenib tablet of the present embodiment includes a tablet core and a coating, and the tablet core is mainly composed of the following components in parts by weight: 41.5 parts of regorafenib monohydrate (calculated as regorafenib 40 parts), microcrystalline cellulose PH101100 parts, croscarmellose sodium 160 parts, povidone K25160 parts, silicon dioxide 3 parts, magnesium stearate 4 parts; The quality of described coating is tablet core 2.92% of the mass; the coating is mainly composed of coating material and colorant, the coating material is a gastric-soluble film coating premix, and the colorant is red iron oxide; the gastric-soluble film coating premix and The mass ratio of red iron oxide is 13.962:0.093.

[0056] The preparation method of the regorafenib tablet of the present embodiment comprises the following steps:

[0057] 1) Get regorafenib of 40 parts by weight and the povidone K25 of 160 parts by weight, be dissolved in the mixed solvent that the mas...

Embodiment 2

[0068] The regorafenib tablet of the present embodiment includes a tablet core and a coating, and the tablet core is mainly composed of the following components in parts by weight: 41.5 parts of regorafenib monohydrate (calculated as regorafenib 40 parts), microcrystalline cellulose PH101100 parts, croscarmellose sodium 160 parts, povidone K25160 parts, silicon dioxide 3 parts, magnesium stearate 4 parts; The quality of described coating is tablet core 2.58% of the mass; the coating is mainly composed of coating material and coloring agent, and the coating material is a gastric-soluble film coating premix, and the colorant is red iron oxide; the gastric-soluble film coating premix and The mass ratio of red iron oxide is 12:0.08.

[0069] The preparation method of the regorafenib tablet of the present embodiment comprises the following steps:

[0070] 1) Get regorafenib of 40 parts by weight and the povidone K25 of 160 parts by weight, be dissolved in the mixed solvent that th...

Embodiment 3

[0090]The regorafenib tablet of the present embodiment includes a tablet core and a coating, and the tablet core is mainly composed of the following components in parts by weight: 41.5 parts of regorafenib monohydrate (calculated as regorafenib 40 parts), microcrystalline cellulose PH101100 parts, croscarmellose sodium 160 parts, povidone K25160 parts, silicon dioxide 3 parts, magnesium stearate 4 parts; The quality of described coating is tablet core 2.58% of the mass; the coating is mainly composed of coating material and coloring agent, and the coating material is a gastric-soluble film coating premix, and the colorant is red iron oxide; the gastric-soluble film coating premix and The mass ratio of red iron oxide is 12:0.08.

[0091] The preparation method of the regorafenib tablet of the present embodiment comprises the following steps:

[0092] 1) Get regorafenib of 40 parts by weight and the povidone K25 of 160 parts by weight, be dissolved in the mixed solvent that the...

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Abstract

The invention discloses stivarga tablets and a preparation method thereof. The stivarga tablets are mainly prepared from, by weight, 40 parts of stivarga, 100 parts of microcrystalline cellulose, 160 parts of croscarmellose sodium, 160 parts of povidone, 3 parts of silicon dioxide and 4 parts of magnesium stearate. With stivarga as an active pharmaceutical ingredient, microcrystalline cellulose as a filling agent, croscarmellose sodium as a disintegrating agent, povidone as a solid dispersion carrier and a binder, silicon dioxide as a glidant and magnesium stearate as a lubricant, the stivarga tablets are obtained by reasonably adjusting the dosage of each component. The tablets have the advantages of being stable in nature and high in dissolution rate and bioavailability, and are mainly used for treating the metastatic colorectal cancer, the gastrointestinal stromal tumor and the like.

Description

technical field [0001] The invention belongs to the technical field of regorafenib pharmaceutical compositions, in particular to a regorafenib tablet, and also relates to a preparation method of the regorafenib tablet. Background technique [0002] Regorafenib, CAS number: 1019206-88-2, chemical name: 4-{4-[3-(4-chloro-3-trifluoromethyl-phenyl)-ureide]-3- Fluorophenoxy}-pyridine-2-carboxylic acid methylamine. Regorafenib is a potent anticancer and antiangiogenic agent with various activities, including inhibitory activity against VEGFR, PDGFR, raf, p38 and / or flt-3 kinase signaling molecules, and it is useful in the treatment of Various diseases and conditions, such as hyperproliferative diseases, such as cancer, tumor, lymphoma, sarcoma, and leukemia, are mainly used in the treatment of metastatic colorectal cancer, gastrointestinal stromal tumor, etc. [0003] What is commonly used in the prior art is regorafenib monohydrate, molecular formula is C 21 h 15 CIF 4 N 4 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K9/28A61K31/44A61K47/38A61K47/32A61K47/04A61K47/12A61P35/04A61P35/00
CPCA61K9/2009A61K9/2013A61K9/2027A61K9/2054A61K9/2813A61K31/44
Inventor 靳勇郭海波
Owner HENAN RUNHONG PHARMA